Sitagliptin, known by the chemical name 3(R)-Amino-1-[3-(trifluoromethyl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one phosphate, modulates the enzyme dipeptidyl-peptidase IV (DPP-IV).
Sitagliptin is currently used in the treatment of Type II diabetes. It is also in clinical trials for lowering of fasting glucose levels.
Accordingly, it is desirable to provide a compound that has the beneficial activities of sitagliptin and may also have other benefits, e.g., reduced adverse side effects, with a decreased metabolic liability, to further extend its pharmacological effective life, enhance patient compliance and, potentially, to decrease population pharmacokinetic variability and/or decrease its potential for dangerous drug-drug interactions.